AR050945A1 - MEDICATIONS CONTAINING CARBON COMPOUNDS AND THEIR USE - Google Patents

MEDICATIONS CONTAINING CARBON COMPOUNDS AND THEIR USE

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Publication number
AR050945A1
AR050945A1 ARP050103944A ARP050103944A AR050945A1 AR 050945 A1 AR050945 A1 AR 050945A1 AR P050103944 A ARP050103944 A AR P050103944A AR P050103944 A ARP050103944 A AR P050103944A AR 050945 A1 AR050945 A1 AR 050945A1
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Argentina
Prior art keywords
mono
atoms
hal
coor3
het
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ARP050103944A
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Spanish (es)
Inventor
Dieter Dorsch
Werner Mederski
Christos Tsaklakidis
Johannes Gleitz
Bertram Cezanne
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Merck Patent Gmbh
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Publication of AR050945A1 publication Critical patent/AR050945A1/en

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    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
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    • A61P31/04—Antibacterial agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Uso de compuesto de la formula (1), en la que: R1, R2 son cada uno, de modo independiente entre sí, H, =O, Hal, A, etinilo, OR3, N(R3)2, NO2, CN, N3, COOR3, CON(R3)2, -[C(R4)2]n-Ar, -[C(R4)2]n-Het, -[C(R4)2]n-cicloalquilo, -OCOR3, -OCON(R3)2, NR3COA o NR3SO2A; R1 y R2 también son juntos un carbociclo o heterociclo de 3 a 7 miembros unidos de forma bicíclica o espirocíclica con 0 a 3 átomos de N, O y/o S; R3 es H, A, H-C:::C-CH2-, CH3-C:::C-CH2-, -CH2-CH(OH)-CH2OH, -CH2-CH(OH)-CH2NH2, -CH2- CH(OH)-CH2Het', -[C(R4)2]n-Ar', -[C(R4)2]n-Het', -[C(R4)2]n-cicloalquilo, -[C(R4)2]n-COOA o -[C(R4)2]nN(R4)2; R4 es H o A; W es N, CR3 o un átomo de C sp2 hibridado; E es junto con W un anillo carbocíclico o heterocíclico saturado de 3 a 7 miembros con 0 a 3 átomo de N, 0 a 2 átomo de O y/o 0 a 2 átomos de S, que puede contener un enlace doble; D es un carbociclo o heterociclo aromático mono- o bicíclico no sustituido o mono- o polisustituido con Hal, A, OR3, N(R3)2, NO2, CN, COOR3 o CON(R3)2, con 0 a 4 átomos de N, O y/o S; G es -[C(R4)2]n-, -[C(R4)2]nNR3, -[C(R4)2]nO-, -[C(R4)2]nS- o -[C(R4)=C(R4)]n-; X es -[C(R4)2]nCONR3[C(R4)2]n-, -[C(R4)2]nNR3CO[C(R4)2]n-; -[C(R4)2]nNR3[C(R4)2]n-, -[C(R4)2]nO[C(R4)2]n-, -[C(R4)2]nCO[C(R4)2]n- o - [C(R4)2]nCOO[C(R4)2]n-; Y es alquileno, cicloalquileno, Het-diílo o Ar-diílo; T es un carbociclo o heterociclo mono- o bicíclico saturado o insaturado con 0 a 4 átomos de N, O y/o S, que está mono- o disustituido con =O, =S, =NR3, =N-CN, =N-NO2, =NOR3, =NCOR3, =NCOOR3, =NOCOR3 y que también puede estar mono-, di- o trisustituido con R3, Hal, A, -[C(R4)2]n-Ar, -[C(R4)2]n-Het, -[C(R4)2]n-cicloalquilo, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2NR3 y/o S(O)nA; A es alquilo no ramificado o ramificado con C1-10, en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupos -CH=CH y/o también 1-7 átomos de H pueden estar reemplazados por F; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2, S(O)nA, -[C(R4)2]n-COOR3 u -O[C(R4)2]o-COOR3; Ar' es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, OR4, N(R4)2, NO2, CN, COOR4, CON(R4)2, NR4COA, NR4CON(R4)2, NR4SO2A, COR4, SO2N(R4)2, S(O)nA, -[C(R4)2]n-COOR4 u -O[C(R4)2]o-COOR4; Het es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar no sustituido o mono-, di- o trisustituido con Hal, A; -[C(R4)2]n-Ar, -[C(R4)2]n-Het', -[C(R4)2]n-cicloalquilo, OR3, N(R3)2, NR3CON(R3)2, NO2, CN, -[C(R4)2]n-COOR3, -[C(R4)2]n-CON(R3)2, NR3COA, NR3SO2A, COR3, SO2NR3, S(O)mA y/o el oxígeno del carbonilo; Het' es un heterociclo mono-, o bicíclico saturado, insaturado o aromático con 1 a 4 átomo de N, O y/o S, que puede estar no sustituido o mono- o disustituido con el oxígeno del carbonilo, =S, =N(R4)2, Hal, A, OR4, N(R4)2, NO2, CN, COOR4, CON(R4)2, NR4COA, NR4CON(R4)2, NR4SO2A, COR4, SO2NR4 y/o S(O)nA; Hal es F, Cl, Br o I; n es 0, 1 o 2; o es 1, 2 o 3; así como sus derivados, solvatos, sales y estereoisomeros de utilidad farmacéuticamente, incluyendo sus mezclas en todas las proporciones, para preparar un medicamento para la prevencion y el tratamiento de enfermedades tromboembolicas y/o trombosis como consecuencia de una intervencion quirurgica, enfermedades de origen genético con tendencia incrementada a la trombosis, enfermedades del sistema vascular arterial y venoso, insuficiencia cardíaca, fibrilacion atrial, trombofilia, tinnitus y/o sepsis.Use of compound of the formula (1), in which: R1, R2 are each, independently of each other, H, = O, Hal, A, ethynyl, OR3, N (R3) 2, NO2, CN, N3, COOR3, CON (R3) 2, - [C (R4) 2] n-Ar, - [C (R4) 2] n-Het, - [C (R4) 2] n-cycloalkyl, -OCOR3, - OCON (R3) 2, NR3COA or NR3SO2A; R1 and R2 are also together a 3- to 7-membered carbocycle or heterocycle linked in a bicyclic or spirocyclic form with 0 to 3 atoms of N, O and / or S; R3 is H, A, HC ::: C-CH2-, CH3-C ::: C-CH2-, -CH2-CH (OH) -CH2OH, -CH2-CH (OH) -CH2NH2, -CH2- CH (OH) -CH2Het ', - [C (R4) 2] n-Ar', - [C (R4) 2] n-Het ', - [C (R4) 2] n-cycloalkyl, - [C (R4 ) 2] n-COOA or - [C (R4) 2] nN (R4) 2; R4 is H or A; W is N, CR3 or a hybridized C sp2 atom; E is together with W a saturated carbocyclic or heterocyclic ring of 3 to 7 members with 0 to 3 atoms of N, 0 to 2 atoms of O and / or 0 to 2 atoms of S, which may contain a double bond; D is a mono- or bicyclic aromatic carbocycle or heterocycle unsubstituted or mono- or polysubstituted with Hal, A, OR3, N (R3) 2, NO2, CN, COOR3 or CON (R3) 2, with 0 to 4 N atoms , O and / or S; G is - [C (R4) 2] n-, - [C (R4) 2] nNR3, - [C (R4) 2] nO-, - [C (R4) 2] nS- or - [C (R4 ) = C (R4)] n-; X is - [C (R4) 2] nCONR3 [C (R4) 2] n-, - [C (R4) 2] nNR3CO [C (R4) 2] n-; - [C (R4) 2] nNR3 [C (R4) 2] n-, - [C (R4) 2] nO [C (R4) 2] n-, - [C (R4) 2] nCO [C ( R4) 2] n- or - [C (R4) 2] nCOO [C (R4) 2] n-; Y is alkylene, cycloalkylene, Het-diyl or Ar-diyl; T is a saturated or unsaturated mono- or bicyclic carbocycle or heterocycle with 0 to 4 atoms of N, O and / or S, which is mono- or disubstituted with = O, = S, = NR3, = N-CN, = N -NO2, = NOR3, = NCOR3, = NCOOR3, = NOCOR3 and which can also be mono-, di- or trisubstituted with R3, Hal, A, - [C (R4) 2] n-Ar, - [C (R4 ) 2] n-Het, - [C (R4) 2] n-cycloalkyl, OR3, N (R3) 2, NO2, CN, COOR3, CON (R3) 2, NR3COA, NR3CON (R3) 2, NR3SO2A, COR3 , SO2NR3 and / or S (O) nA; A is unbranched or branched C1-10 alkyl, wherein one or two CH2 groups may be replaced by O or S atoms and / or by groups -CH = CH and / or 1-7 H atoms may be replaced by F; Ar is phenyl, naphthyl or biphenyl unsubstituted or mono-, di- or trisubstituted with Hal, A, OR3, N (R3) 2, NO2, CN, COOR3, CON (R3) 2, NR3COA, NR3CON (R3) 2, NR3SO2A, COR3, SO2N (R3) 2, S (O) nA, - [C (R4) 2] n-COOR3 or -O [C (R4) 2] or -COOR3; Ar 'is phenyl, naphthyl or biphenyl unsubstituted or mono-, di- or trisubstituted with Hal, A, OR4, N (R4) 2, NO2, CN, COOR4, CON (R4) 2, NR4COA, NR4CON (R4) 2 , NR4SO2A, COR4, SO2N (R4) 2, S (O) nA, - [C (R4) 2] n-COOR4 or -O [C (R4) 2] or -COOR4; Het is a saturated, unsaturated or aromatic mono- or bicyclic heterocycle with 1 to 4 atoms of N, O and / or S, which may be unsubstituted or mono-, di- or trisubstituted with Hal, A; - [C (R4) 2] n-Ar, - [C (R4) 2] n-Het ', - [C (R4) 2] n-cycloalkyl, OR3, N (R3) 2, NR3CON (R3) 2 , NO2, CN, - [C (R4) 2] n-COOR3, - [C (R4) 2] n-CON (R3) 2, NR3COA, NR3SO2A, COR3, SO2NR3, S (O) mA and / or the carbonyl oxygen; Het 'is a saturated, unsaturated or aromatic mono-, or bicyclic heterocycle with 1 to 4 atoms of N, O and / or S, which may be unsubstituted or mono- or disubstituted with carbonyl oxygen, = S, = N (R4) 2, Hal, A, OR4, N (R4) 2, NO2, CN, COOR4, CON (R4) 2, NR4COA, NR4CON (R4) 2, NR4SO2A, COR4, SO2NR4 and / or S (O) nA ; Hal is F, Cl, Br or I; n is 0, 1 or 2; or is 1, 2 or 3; as well as its derivatives, solvates, salts and stereoisomers useful pharmaceutically, including mixtures in all proportions, to prepare a drug for the prevention and treatment of thromboembolic diseases and / or thrombosis as a result of surgical intervention, diseases of genetic origin with an increased tendency to thrombosis, diseases of the arterial and venous vascular system, heart failure, atrial fibrillation, thrombophilia, tinnitus and / or sepsis.

ARP050103944A 2004-09-22 2005-09-21 MEDICATIONS CONTAINING CARBON COMPOUNDS AND THEIR USE AR050945A1 (en)

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